从异乙酰香草酮出发,经过烷基化、Wittig—Homer、溴代、酞酰亚胺化、不对称还原和脱保护-环化反应6步合成了(R)-咯利普兰,总收率达到了34%。目标产物的结构经过核磁和质谱的确证。
The synthetic method on (R) -rolipram was described in detail. Using isoacetovanitlone as materials, (R) - rolipram was synthesized by six steps of alkylation, Wittig - Homer, bromo reaction, phthalimide, enantioselective conjugate reduction and deprotection followed by cyclization reaction. The product yield was 34%. The structure of the product was determined by ^1H NMR and MS.